Ezetimibe (Chemical Formula a), which is a drug used as an inhibitor of cholesterol absorption in small intestine, is used as a main material of Ezetrol and Vytorin, which are commercially available drugs for the treatment of hyperlipidemia. The ezetimibe synthesis process, developed by Schering-Plough, is problematic because Grignard reagents and organolithium reagents, which are difficult to handle and have a risk of explosion, are used, and moreover, hydrogen gas at 2 atm and 4 atm is used upon reduction and deprotection reactions. Therefore, it is necessary to develop a new reaction capable of progressing under mild conditions to replace the reaction requiring such harsh conditions. [Chemical Formula a]
